CB-839

CB-839 is a potent, selective, and orally bioavailable inhibitor of both splice variants of glutaminase (KGA and GAC); inhibits recombinant GAC with an IC₅₀ of <15 nM. CB-839 displays antiproliferative activity in a triple-negative breast cancer (TNBC) cell line, HCC-1806, that is associated with a marked decrease in glutamine consumption, glutamate production, oxygen consumption, and the steady-state levels of glutathione and several tricarboxylic acid cycle intermediates.